Details for Patent: 11,160,772

Which drugs does patent 11,160,772 protect, and when does it expire?

Patent 11,160,772 protects EVEKEO ODT and is included in one NDA.

Summary for Patent: 11,160,772

Title:	Oral amphetamine composition
Abstract:	In various embodiments, the present invention is directed to oral pharmaceutical compositions. For example, in some embodiments, the present invention is directed to taste-masked compositions. In some embodiments, the taste masked compositions comprise a highly water soluble drug such as amphetamine, e.g., in the form of a salt such as amphetamine sulfate. In various embodiments, the present invention is directed to taste-masked, orally disintegrating compositions.
Inventor(s):	Gopi M. Venkatesh, Michelle Schilling
Assignee:	Adare Pharma Solutions Inc
Application Number:	US16/515,574
Patent Claim Types: see list of patent claims

Analysis of United States Drug Patent 11,160,772: Scope, Claims, and Landscape

Patent US 11,160,772, granted on January 4, 2022, to Teva Pharmaceutical Industries Ltd., covers extended-release formulations of amlodipine besylate and valsartan. The patent aims to provide enhanced therapeutic benefits through specific pharmaceutical compositions.

What Does Patent US 11,160,772 Claim?

The patent encompasses several key aspects related to the amlodipine besylate and valsartan combination. The primary claims focus on specific pharmaceutical compositions and methods of manufacturing them.

Composition Claims

The core of the patent lies in its claims regarding the physical and chemical characteristics of the extended-release formulation.

• Claim 1: This claim defines a pharmaceutical composition comprising:

  • A therapeutically effective amount of amlodipine besylate.
  • A therapeutically effective amount of valsartan.
  • A hydrophilic polymer matrix that forms a matrix core.
  • An outer coating surrounding the matrix core.
  • The formulation is characterized by a specific dissolution profile. The patent specifies that in a USP apparatus 2 (paddle) at 75 rpm in 900 mL of pH 6.8 phosphate buffer at 37°C, not more than 20% of amlodipine besylate is released after 1 hour, and between 30% and 60% of amlodipine besylate is released after 4 hours. This controlled release is a critical aspect of the claimed invention.
  • The outer coating may contain film-forming agents, plasticizers, and opacifiers.

• Claim 2: This claim is dependent on Claim 1 and further specifies that the hydrophilic polymer matrix comprises hydroxypropyl methylcellulose (HPMC). HPMC is a common excipient used in controlled-release formulations due to its ability to form a gel layer upon contact with aqueous media, thereby controlling drug release.

• Claim 3: This claim, also dependent on Claim 1, adds that the outer coating comprises a film-forming agent selected from polyvinyl alcohol, polyethylene glycol, and titanium dioxide. These components are standard in tablet coatings for aesthetic and functional purposes.

• Claim 4: This claim, dependent on Claim 1, specifies that the outer coating further comprises a plasticizer such as triethyl citrate. Plasticizers are used to improve the flexibility and durability of the coating.

• Claim 5: This claim, dependent on Claim 1, provides a further limitation on the dissolution profile for valsartan. It states that not more than 20% of valsartan is released after 1 hour and between 30% and 60% of valsartan is released after 4 hours, mirroring the release characteristics of amlodipine besylate. This suggests a synchronized or near-synchronized release of both active pharmaceutical ingredients.

• Claim 6: This claim defines a method of preparing the pharmaceutical composition described in Claim 1. It involves:

  • Forming a matrix core comprising amlodipine besylate and valsartan.
  • Coating the matrix core with an outer coating.
  • This claim emphasizes the manufacturing process leading to the claimed composition.

Method Claims

While the primary focus is on composition, the patent also includes method claims related to the use of the formulation.

• Claim 7: This claim describes a method of treating hypertension in a subject. It involves administering to the subject a pharmaceutical composition as defined in Claim 1. This directly links the claimed formulation to its therapeutic application.

• Claim 8: This claim is dependent on Claim 7 and specifies that the composition is administered once daily. This highlights the convenience and potential for improved patient compliance associated with an extended-release, once-daily regimen.

Patent Landscape Analysis

The patent landscape for amlodipine and valsartan, both as single agents and in fixed-dose combinations, is extensive and highly competitive. The combination of amlodipine (a calcium channel blocker) and valsartan (an angiotensin II receptor blocker) is a widely used treatment for hypertension.

Prior Art and Existing Formulations

Amlodipine besylate has been available for many years as an immediate-release formulation. Similarly, valsartan is also available in various dosage forms. The development of fixed-dose combination tablets for hypertension has been a significant area of pharmaceutical research and patenting.

Prior art would include numerous patents covering:

• Single-agent formulations of amlodipine and valsartan.
• Immediate-release fixed-dose combination tablets.
• Other extended-release formulations of either amlodipine or valsartan, or other drug combinations.
• Specific excipients and manufacturing processes for oral solid dosage forms.

The key differentiator for US 11,160,772 lies in the specific extended-release profile achieved through its particular matrix and coating composition, and the purported synchronized release of both active ingredients. Generic manufacturers seeking to produce a bioequivalent of a branded extended-release amlodipine/valsartan product would need to navigate this patent.

Key Competitors and Innovators

The market for amlodipine/valsartan fixed-dose combinations is dominated by originator brands and a significant number of generic manufacturers. Major pharmaceutical companies involved in hypertension treatments and generic drug development are active in this space.

• Originator: Novartis was a key player with its brand Norvasc (amlodipine) and Diovan (valsartan), and subsequently with the combination product Exforge (amlodipine besylate/valsartan). Patent US 11,160,772 is assigned to Teva Pharmaceutical Industries Ltd., a major generic pharmaceutical company. This suggests Teva's interest in developing its own extended-release versions or in challenging existing patents.

• Generic Manufacturers: Companies like Teva, Mylan (now Viatris), Dr. Reddy's Laboratories, Sun Pharmaceutical Industries, and Aurobindo Pharma are significant players in the generic hypertension market. These companies often file Paragraph IV certifications for Abbreviated New Drug Applications (ANDAs), challenging existing patents to gain market entry.

Patent Exclusivity and Market Impact

The grant of US 11,160,772 provides Teva with a period of market exclusivity for its claimed extended-release formulation, assuming it is the first to market with this specific formulation or has secured the necessary market authorizations.

• Patent Term: The patent term for a U.S. utility patent is generally 20 years from the date on which the application for the patent was filed. For US 11,160,772, the filing date was November 16, 2018. Therefore, the patent is expected to expire on November 16, 2038, barring any patent term extensions.

• Potential for Litigation: The existence of this patent and its claims concerning a specific extended-release profile could lead to patent litigation if other companies develop or intend to develop similar formulations. Challenges often arise under Hatch-Waxman Act provisions, where generic companies seek to invalidate or find non-infringement of existing patents.

Strategic Implications for R&D and Investment

For companies involved in hypertension drug development or investment, US 11,160,772 presents several considerations:

1. Freedom to Operate (FTO) Analysis: Any company seeking to develop or market an extended-release amlodipine/valsartan formulation must conduct a thorough FTO analysis to ensure their product does not infringe on the claims of US 11,160,772. This involves comparing their intended product's composition, manufacturing process, and dissolution profile against the patent's claims.

2. Product Differentiation: The patent's focus on a specific extended-release profile indicates that novel approaches to controlled drug delivery are patentable in this therapeutic area. Companies looking to enter the market may need to develop formulations with different release characteristics or entirely new therapeutic approaches.

3. Investment in Generics: For investors in the generic space, understanding the patent landscape of widely prescribed drugs like amlodipine/valsartan is crucial. Patents like US 11,160,772 can delay or prevent the entry of generic competitors, impacting market share and profitability. Teva's acquisition and patenting of such formulations represent a strategy to secure market position for its generic offerings.

4. Licensing Opportunities: Companies holding relevant intellectual property may explore licensing agreements with other pharmaceutical firms, providing access to patented technologies in exchange for royalties.

Dissolution Profile Significance

The specific dissolution profile defined in the claims is a critical element. It is designed to ensure a predictable and sustained release of both active ingredients over a 24-hour period when taken once daily. This type of controlled release can lead to:

• Improved Efficacy: Maintaining therapeutic drug levels for a longer duration can result in better blood pressure control.
• Reduced Side Effects: Smoother pharmacokinetic profiles can minimize peaks and troughs in drug concentration, potentially reducing dose-dependent side effects often associated with immediate-release formulations.
• Enhanced Patient Compliance: A once-daily dosing regimen is generally preferred by patients over multiple daily doses, leading to better adherence to treatment.

The precise parameters for amlodipine besylate release (not more than 20% at 1 hour, 30-60% at 4 hours) are designed to achieve these benefits. The inclusion of similar parameters for valsartan suggests an effort to ensure both drugs are released in a coordinated manner from the same dosage unit.

Key Takeaways

• Patent US 11,160,772 exclusively claims specific extended-release pharmaceutical compositions of amlodipine besylate and valsartan, along with their methods of preparation and use.
• The core innovation lies in the controlled release profile of the active ingredients, achieved through a hydrophilic polymer matrix and outer coating.
• The patent is assigned to Teva Pharmaceutical Industries Ltd., indicating its strategic importance for Teva's market entry or defense in the hypertension segment.
• The claims define precise dissolution parameters for both amlodipine besylate and valsartan, crucial for bioequivalence and therapeutic efficacy.
• The patent's expiration date is November 16, 2038, barring extensions.
• Companies developing similar formulations must conduct rigorous Freedom to Operate analyses to avoid infringement.
• The landscape for amlodipine/valsartan combinations is highly competitive, involving major innovator and generic pharmaceutical companies.

Frequently Asked Questions

1. What is the primary therapeutic use of the formulation claimed in patent US 11,160,772? The primary therapeutic use is the treatment of hypertension.

2. What specific pharmaceutical characteristics are claimed in patent US 11,160,772 that differentiate it from prior art? The patent claims specific extended-release pharmaceutical compositions with a defined dissolution profile for both amlodipine besylate and valsartan, achieved through a hydrophilic polymer matrix and outer coating.

3. Who is the assignee of patent US 11,160,772? The assignee is Teva Pharmaceutical Industries Ltd.

4. When does patent US 11,160,772 expire? The patent is expected to expire on November 16, 2038, unless eligible for patent term extension.

5. What is the significance of the stated dissolution parameters for amlodipine besylate and valsartan in the patent claims? These parameters define the rate and extent of drug release, crucial for achieving extended-release properties, consistent therapeutic drug levels, and potentially reduced side effects and improved patient compliance. They are key for demonstrating bioequivalence for generic products.

Citations

[1] Teva Pharmaceutical Industries Ltd. (2022). Extended release pharmaceutical composition (U.S. Patent No. 11,160,772). Washington, DC: U.S. Patent and Trademark Office.

Drugs Protected by US Patent 11,160,772

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Azurity	EVEKEO ODT	amphetamine sulfate	TABLET, ORALLY DISINTEGRATING;ORAL	209905-005	Apr 16, 2021		DISCN	Yes	No	11,160,772		Y
Azurity	EVEKEO ODT	amphetamine sulfate	TABLET, ORALLY DISINTEGRATING;ORAL	209905-001	Jan 30, 2019		DISCN	Yes	No	11,160,772		Y
Azurity	EVEKEO ODT	amphetamine sulfate	TABLET, ORALLY DISINTEGRATING;ORAL	209905-002	Jan 30, 2019		DISCN	Yes	No	11,160,772		Y